Spiroheptane as a Saturated Benzene Bioisostere

The spiro[3.3]heptane core, with the non‐coplanar exit vectors, was shown to be a saturated benzene bioisostere. This scaffold was incorporated into the anticancer drug sonidegib (instead of the meta‐benzene), the anticancer drug vorinostat (instead of the phenyl ring), and the anesthetic drug benzo...

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Bibliographic Details
Published in:	Angewandte Chemie Vol. 136; no. 9
Main Authors:	Prysiazhniuk, Kateryna, Datsenko, Oleksandr P, Polishchuk, Oleksandr, Shulha, Stanislav, Shablykin, Oleh, Nikandrova, Yelyzaveta, Horbatok, Kateryna, Bodenchuk, Iryna, Petro Borysko, Shepilov, Dmytro, Pishel, Iryna, Kubyshkin, Vladimir, Mykhailiuk, Pavel K
Format:	Journal Article
Language:	English
Published:	Weinheim Wiley Subscription Services, Inc 01-02-2024
Subjects:	Antineoplastic drugs Benzene Heptanes
Online Access:	Get full text
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Summary:	The spiro[3.3]heptane core, with the non‐coplanar exit vectors, was shown to be a saturated benzene bioisostere. This scaffold was incorporated into the anticancer drug sonidegib (instead of the meta‐benzene), the anticancer drug vorinostat (instead of the phenyl ring), and the anesthetic drug benzocaine (instead of the para‐benzene). The patent‐free saturated analogs obtained showed a high potency in the corresponding biological assays.Dedicated to the people of Ukraine
ISSN:	0044-8249 1521-3757
DOI:	10.1002/ange.202316557